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Serum concentrations of amiodarone during long term therapy. Relation to dose, efficacy and toxicity

Summary

In 17 patients on long term therapy with amiodarone, serum drug levels measured by HPLC were related to pharmacological effects. At steady state, serum levels were directly proportional to the dose, 5 mg/kg per day leading to an average serum level of approximately 2.5 µmol/l. The non-amiodarone level of iodine averaged 4-times higher than the level of amiodarone iodine. The elimination half-life of amiodarone ranged from 21 to 78 days, and of non-amiodarone iodine from 24 to 160 days. Control of arrhythmias was satisfactory in all 12 evaluable patients, when the serum amiodarone level exceeded 1.5 µmol/l. Deterioration of vision and polyserositis occurred only at amiodarone levels above 4 µmol/l. Tentatively, a therapeutic range of 1.5 to 4 µmol/l is proposed. In contrast, thyroid dysfunction was observed at any amiodarone level. In view of the narrow therapeutic window, therapy with amiodarone may be optimized by monitoring its serum level and in addition, thyroid function should be regularly checked.

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Stäubli, M., Bircher, J., Galeazzi, R.L. et al. Serum concentrations of amiodarone during long term therapy. Relation to dose, efficacy and toxicity. Eur J Clin Pharmacol 24, 485–494 (1983). https://doi.org/10.1007/BF00609891

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Key words

  • amiodarone
  • pharmacokinetics
  • therapeutic serum level
  • thyroid function
  • antiarrhythmic therapy
  • adverse effects